中国中医药信息杂志
中國中醫藥信息雜誌
중국중의약신식잡지
CHINESE JOURNAL OF INFORMATION ON TRADITIONAL CHINESE MEDICINE
2015年
9期
79-82
,共4页
护肠清毒微丸%大黄素%结肠靶向%药物动力学
護腸清毒微汍%大黃素%結腸靶嚮%藥物動力學
호장청독미환%대황소%결장파향%약물동역학
Huchang Qingdu Pellets%emodin%colon targeting%pharmacokinetics
目的：建立护肠清毒微丸灌胃后大鼠血浆和结肠组织中大黄素浓度高效液相色谱测定方法,探讨试验微丸在大鼠体内药物动力学性质及结肠组织分布情况。方法将Wistar大鼠随机分为微丸组和普通胶囊组,分别予护肠清毒微丸和胶囊内容物灌胃后,于给定的时间点(1、2、3、4、5、6、8、12、24 h)从大鼠静脉窦取血分析。处死大鼠,分离结肠组织,进行提取分析。色谱条件：Phenomenex C18柱(4.6 mm×150 mm,10μm),流动相为甲醇-0.1%冰醋酸溶液(80∶20),流速1 mL/min,检测波长254 nm。结果大黄素在0.102～20.40μg/mL范围内线性关系良好。回归方程分别为：血浆溶液A＝76825C＋3567.8,r＝0.9994(n＝6)；结肠组织溶液A＝75931C＋3384.2,r＝0.9990(n＝6)。日间精密度和日内精密度均＜4.0%,提取回收率＞90.0%。微丸组大鼠血液和结肠组织中所含大黄素的药物动力学参数 T1/2和 Tmax较普通胶囊组有所延长,Cmax和 AUC0-24较普通胶囊组明显提高。结论护肠清毒微丸具有控释和结肠靶向的作用。
目的：建立護腸清毒微汍灌胃後大鼠血漿和結腸組織中大黃素濃度高效液相色譜測定方法,探討試驗微汍在大鼠體內藥物動力學性質及結腸組織分佈情況。方法將Wistar大鼠隨機分為微汍組和普通膠囊組,分彆予護腸清毒微汍和膠囊內容物灌胃後,于給定的時間點(1、2、3、4、5、6、8、12、24 h)從大鼠靜脈竇取血分析。處死大鼠,分離結腸組織,進行提取分析。色譜條件：Phenomenex C18柱(4.6 mm×150 mm,10μm),流動相為甲醇-0.1%冰醋痠溶液(80∶20),流速1 mL/min,檢測波長254 nm。結果大黃素在0.102～20.40μg/mL範圍內線性關繫良好。迴歸方程分彆為：血漿溶液A＝76825C＋3567.8,r＝0.9994(n＝6)；結腸組織溶液A＝75931C＋3384.2,r＝0.9990(n＝6)。日間精密度和日內精密度均＜4.0%,提取迴收率＞90.0%。微汍組大鼠血液和結腸組織中所含大黃素的藥物動力學參數 T1/2和 Tmax較普通膠囊組有所延長,Cmax和 AUC0-24較普通膠囊組明顯提高。結論護腸清毒微汍具有控釋和結腸靶嚮的作用。
목적：건립호장청독미환관위후대서혈장화결장조직중대황소농도고효액상색보측정방법,탐토시험미환재대서체내약물동역학성질급결장조직분포정황。방법장Wistar대서수궤분위미환조화보통효낭조,분별여호장청독미환화효낭내용물관위후,우급정적시간점(1、2、3、4、5、6、8、12、24 h)종대서정맥두취혈분석。처사대서,분리결장조직,진행제취분석。색보조건：Phenomenex C18주(4.6 mm×150 mm,10μm),류동상위갑순-0.1%빙작산용액(80∶20),류속1 mL/min,검측파장254 nm。결과대황소재0.102～20.40μg/mL범위내선성관계량호。회귀방정분별위：혈장용액A＝76825C＋3567.8,r＝0.9994(n＝6)；결장조직용액A＝75931C＋3384.2,r＝0.9990(n＝6)。일간정밀도화일내정밀도균＜4.0%,제취회수솔＞90.0%。미환조대서혈액화결장조직중소함대황소적약물동역학삼수 T1/2화 Tmax교보통효낭조유소연장,Cmax화 AUC0-24교보통효낭조명현제고。결론호장청독미환구유공석화결장파향적작용。
Objective To establish an HPLC method for concentration determination of emodin in plasma and colon tissues after gavage withHuchang Qingdu Pellets;To explore pharmacokinetic properties and colon tissue distribution ofHuchang Qingdu Pellets in rats.Methods Wistar rats were randomly divided into Pellets group and ordinary capsule group. Blood was taken after gavage withHuchang QingduPellets or capsule content in given time points (1, 2, 3, 4, 5, 6, 8, 12, 24 h) from rat venous sinus and analyzed. Rats were put to death, and gastric and colon tissues were isolated and extracted for analysis. Chromatographic conditions:Phenomenex C18 column (4.6 mm × 150 mm, 10μm), the mobile phase of methanol-0.1% acetic acid solution (80∶20), flow rate of 1 mL/min, the detection wavelength of 254 nm.Results Emodin was in good linear range of 0.102-20.40μg/mL. The regression equations were:plasma solutionA=76 825C + 3567.8,r=0.999 4 (n=6);intestinal tissue solutionA=75 931C + 3384.2,r=0.999 0 (n=6). Day-to-day precision and within-day precision were less than 4%. The recovery rate was more than 90%. Pharmacokinetic parameters of T1/2 and Tmax of emodin in rat blood and intestinal tissues increased compared with the ordinary capsule group;Cmax and AUC0-24 were obviously improved compared with the ordinary capsule group.ConclusionHuchang Qingdu Pellets do have controlled release and colon targeting effect.
